1103524-20-4Relevant academic research and scientific papers
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists
Bharate, Sandip B.,Rodge, Atish,Joshi, Rajendra K.,Kaur, Jaspreet,Srinivasan, Shaila,Senthil Kumar,Kulkarni-Almeida, Asha,Balachandran, Sarala,Balakrishnan, Arun,Vishwakarma, Ram A.
scheme or table, p. 6357 - 6361 (2009/10/01)
In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxyls were synthesized and evaluated for GPR40 agonism using functional calcium-flux assay. Out of 17 compounds evaluated, 14, 17, 19 and 25 exhibited good GPR40 agonistic activity with EC50 values ranging from 0.07 to 8 μM (pEC50 7.12-5.09), respectively, with maximal agonistic response of 84-102%.
